Design and synthesis of novel peptidomimetics for cancer immunotherapy

IF 1.7 Q3 CHEMISTRY, ORGANIC Organic Communications Pub Date : 2020-07-01 DOI:10.25135/ACG.OC.86.20.09.1802
Ceyda Köse, Esra Uysal, B. Yazici, Z. Tuğay, Serap İpek Dingiş Birgül, Hamdullah Yanık, E. Tavukçuoğlu, Sevgi Gulyuz, A. Akdemir, G. Esendagli, Ö. Yılmaz, Onur Alptürk
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引用次数: 1

Abstract

Tumor cells benefit from some certain signals, which are referred to as “immune checkpoints”, to escape immune-mediated destruction. With that in mind, it is believed that the blockade of these points, such as programmed cell death Ligand-1 (PD-L1) and programmed cell death 1 (PD-1), can restore an adaptative immune response against tumoral cells. In this study, we have designed and synthesized some novel peptidomimetics with a 2-aminobenzathiazole scaffold, which targets the PD-1/PDL-1 pathway. In the viability assay, it was found that these compounds decreased the proliferation of peripheral blood mononuclear cells in the concentration of 10 uM. Overall, our results indicate that these novel compounds are potential checkpoint inhibitors for cancer immunotherapy.
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癌症免疫治疗新型拟肽药物的设计与合成
肿瘤细胞受益于一些被称为“免疫检查点”的特定信号,以逃避免疫介导的破坏。考虑到这一点,相信阻断这些点,如程序性细胞死亡配体-1(PD-L1)和程序性细胞死亡率1(PD-1),可以恢复针对肿瘤细胞的适应性免疫反应。在本研究中,我们设计并合成了一些具有2-氨基苄唑支架的新型拟肽制剂,该支架靶向PD-1/PDL-1通路。在活力测定中,发现这些化合物在浓度为10μM时降低了外周血单核细胞的增殖。总体而言,我们的结果表明,这些新化合物是癌症免疫疗法的潜在检查点抑制剂。
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来源期刊
Organic Communications
Organic Communications CHEMISTRY, ORGANIC-
CiteScore
2.80
自引率
11.80%
发文量
21
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